.beta.-Lactam antibacterial agents, their use in pharmaceutical compositions, and intermediates
US4282236A · kind A · utility
Assignee
Inventor
Key dates
| Filing date | Nov 7, 1979 |
| Grant date | Aug 4, 1981 |
| Priority date | — |
| Expiry date | Nov 7, 1999 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07F9/568
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The compounds of the formula (II): ##STR1## and salts and cleavable esters thereof wherein R.sub.1 is a hydrogen atom or a lower alkyl group and R.sub.2 is a CN or CO.sub.2 R.sub.3 group where R.sub.3 is a hydrogen atom or a lower alkyl, aryl, or aralkyl group are antibacterially effective compounds. Their preparation and use is described. R. B. Woodward (Acta Pharm. Suecica 1977, 14 Suppl., p 23-25) disclosed that the compounds of the formula (I): ##STR2## where R was an unspecified group possessed antibacterial activity. No aid in determining the nature of the group R was given by Professor Woodward nor did he describe the preparation of any compounds of the formula (I). However, at the symposium on Current Topics in Drug Research (Uppsala, Sweden October 1977) Professor Woodward described the compound of the formula (I) wherein R is a hydrogen atom. We have prepared this compound and found it to possess a somewhat disappointing degree of antibactrial activity. Clearly it would be desirable to find a class of compound that possess a better degree of activity especially against Gram-positive organisms such as Staphylococcus aureus, Streptococcus pneumoniae or Streptococcus pyogene…
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.